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Pharmaceutical formulations of potassium atp channel openers and uses thereof

A preparation and channel technology, applied in drug delivery, pharmaceutical formulations, etc., can solve problems such as limiting practicability

Inactive Publication Date: 2007-09-26
ESSENTIALIS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The adverse side effects of oral diazoxide limit the usefulness of this drug in the treatment of obese patients at doses in the label range of 3 to 8 mg / kg per day

Method used

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  • Pharmaceutical formulations of potassium atp channel openers and uses thereof
  • Pharmaceutical formulations of potassium atp channel openers and uses thereof
  • Pharmaceutical formulations of potassium atp channel openers and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0450] A. Preparations containing potassium ATP channel activator:

[0451] 1. Compressed tablet preparation

[0452] Combine about 15-30% by weight of diazoxide or its derivatives with about 55-80% by weight of hydroxypropyl methylcellulose, about 3-10wt / vol% of ethyl cellulose and by weight Less than 3% each of magnesium stearate (as a lubricant) and talc (as a glidant) are mixed. The mixture was used to prepare the compressed tablets described in Reddy et al., AAPS Pharm Sci Tech 4(4): 1-9 (2003). The tablets can be coated with a film for microparticles as described below.

[0453] A tablet containing 100 mg of diazoxide or its derivatives will also contain about 400 mg of hydroxypropyl cellulose and 10 mg of ethyl cellulose. A tablet containing 50 mg of diazoxide or its derivatives will also contain about 200 mg of hydroxypropyl cellulose and 50 mg of ethyl cellulose. A tablet containing 25 mg of diazoxide or its derivatives will also contain about 100 mg of hydroxypropyl cell...

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Abstract

Provided are immediate or prolonged administration of certain potassium ATP (KATP) channel openers to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of KATP channel openers that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering KATP channel openers with other drugs to treat diseases of humans and animals.

Description

Invention field [0001] The present invention relates to potassium ATP (K) for the treatment of various diseases and disorders such as diabetes and obesity ATP ) Pharmaceutical preparations of channel openers and their applications. Background of the invention [0002] The following description about the background of the invention is provided only to facilitate the understanding of the invention, and is not admitted to describe or constitute the prior art of the invention. [0003] ATP-sensitive potassium (K ATP ) Channels play an important role in various tissues by combining cell metabolism with bioelectrical activities. This K ATP The channel has been identified as an octameric complex of two unrelated proteins assembled in a 4:4 stoichiometry. The first is the channel formation subunit: Kir6.x, which forms the internally rectified K + Channel; the second is the ABC (ATP binding cassette) transporter, also known as the sulfonylurea receptor (SURx) (Babenko et al., Annu. Rev. P...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K9/22
Inventor 尼尔·M·科文肯尼思·B·卡施金
Owner ESSENTIALIS INC
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